专利号:US-9000209-B2 优先权日:2011-07-22 标题:Method of regioselective synthesis of substituted benzoates 发明人:KRAUS GEORGE A 权利人:KRAUS GEORGE A; UNIV IOWA STATE RES FOUND INC 摘要:A method of synthesis of para-substituted benzoate esters and acids is provided, wherein the para-substituted regioisomer is obtained substantially free of the meta-substituted impurity, the method comprising contacting a coumalate ester or acid and an unactivated alkene at elevated temperature in the presence of a metal oxidation catalyst and an oxidant. The metal oxidation catalyst can be palladium, such as palladium on carbon, and the oxidant can be the oxygen gas in ambient air. The reaction can be carried out without solvent or in high boiling hydrocarbon solvents such as mesitylene. When the unactivated alkene is a monosubstituted alkene, yields of at least about 50 or 60% of para-substituted ester and acid products, respectively, are obtained, substantially free of the regioisomeric meta-substituted impurity.
专利号:US-8114993-B2 优先权日:2007-02-06 标题:Use of aryl chlorides in palladium-catalyzed C-H bond functionalization 发明人:DAUGULIS OLAFS; CHIONG HENDRICH 权利人:DAUGULIS OLAFS; CHIONG HENDRICH; UNIV HOUSTON SYSTEM 摘要:A one-step method for efficiently converting carbon-hydrogen bonds into carbon-carbon bonds using chloroarenes and palladium catalysts is disclosed. This method allows faster introduction of complex molecular entities, a process that would otherwise require many more steps. This invention is particularly relevant for the organic synthesis of complex molecules such as, but not limited to, pharmacophores.
专利号:WO-2021123883-A1 优先权日:2019-12-19 标 题 :Macrocyclic amides acting as plasmepsin inhbitors for the treatment of malaria 发明人:JIRGENSONS AIGARS; KOVADA VADIMS; BOBROVS RAITIS; SUNA EDGARS; JAUDZEMS KRISTAPS; RASINA DACE; ZOGOTA RIMANTS 权利人:LATVIAN INST ORGANIC SYNTHESIS 摘要:The present invention relates to medicine and in particular to the treatment of malarial infections, more particularly to inhibitors of malarial aspartic proteases - plasmepsins. Even more particularly, the invention relates to macrocyclic amides and pharmaceutical compositions thereof and their use as inhibitors for plasmepsins (Plm).
专利号:US-2007265419-A1 优先权日:2006-05-10 标 题:Process for driving gas blowers or fans in a solid-state polymerization process using steam from a terephthalic acid plant 发明人:BONNER RICHARD G; DEBENPORT ALBERT B 权利人:BONNER RICHARD G; DEBENPORT ALBERT B 摘要:A method for integrating energy resources between a process for synthesizing terephthalic acid and a process for the solid-state polymerization of a polyester, which comprises generating steam from the synthesis of terephthalic acid, providing the steam to a condensing turbine to generate power, applying the power to a gas blower or fan to create a stream of gas and applying the stream of gas to fluidize polyester pellets in a crystallization and/or solid-state polymerization process.
专利号:US-8653223-B2 优先权日:2008-04-16 标题:Transketalized compositions, synthesis, and applications 发明人:SELIFONOV SERGEY; GOETZ ADAM EDWARD; JING FENG 权利人:SELIFONOV SERGEY; GOETZ ADAM EDWARD; JING FENG; SEGETIS INC 摘要:Ketal compounds of the structure I n nand a method of preparation of the compound from polyols and oxocarboxylates, as well as uses thereof.
专利号:US-8952042-B2 优先权日:2009-08-19 标 题 :FXR (NR1H4) binding and activity modulating compounds 发明人:KREMOSER CLAUS; ABEL ULRICH; STEENECK CHRISTOPH; KINZEL OLAF 权利人:KREMOSER CLAUS; ABEL ULRICH; STEENECK CHRISTOPH; KINZEL OLAF; PHENEX PHARMACEUTICALS AG 摘要:The present invention relates to compounds of formula (1): n nwhere R, A, Q and Z are defined herein, or an enantiomer, diastereomer, tautomer, solvate, prodrug or pharmaceutical acceptable salt thereof. These compounds bind to the NR1H4 receptor (FXR) and act as agonists of the NR1H4 receptor (FXR). The invention further relates to the use of the compounds for the preparation of a medicament for the treatment of diseases and/or conditions through binding of said nuclear receptor by said compounds, and to a process for the synthesis of said compounds.
摘要:Sanford, M. S.; Cook, A., Science of Synthesis: Catalytic Transformations via CH Activation, (2015) 2, 212. 摘要:Melkonyan, F. S.; Gevorgyan, V., Science of Synthesis: Catalytic Transformations via CH Activation, (2015) 1, 57. 摘要:Xu, L., Science of Synthesis: Advances in Organoboron Chemistry towards Organic Synthesis, (2019) 1, 273. 摘要:Fujihara, T., Science of Synthesis: Special Topics, (2022) 1, 384. 参考文献:10.2166/wst.2005.0269 摘要:Gu J-, Li J, Wang Y. Biochemical pathway and degradation of phthalate ester isomers by bacteria. 2005 Oct 01;52(8):241–8. doi: 10.2166/wst.2005.0269.